Painkillers are the most frequently prescribed group of drugs in clinical practice. Their appropriate selection allows for the reduction of side effects, and also improves the effectiveness of use. The pain itself is a physiological sensation, it plays a warning and protective role. It often happens that the constant pain is one of the causes of the destruction of our psyche … The surface of the skin and most of the mucosa, as well as numerous tissues and internal organs are sensitive to pain stimuli.
For example, the brain and liver are devoid of pain receptors. We distinguish between receptor (nociceptive) pain, which may be somatic, e.g. bone pain or pain resulting from damage to the skin, subcutaneous tissue or muscles, and visceral pain from internal organs. In contrast, non-receptor (neuropathic) pain is attributed to chronic pain caused by damage to the central nervous system as a result of trauma, infection, ischemia, hypoxia, metabolic disorders, or neoplastic infiltration.
When selecting painkillers, several aspects should be taken into account relating to the risk of side effects, interactions, pharmacokinetic properties, as well as the intensity or cause of pain.
Non-opioid analgesics are usually used in the case of pathophysiological pain of inflammatory origin.
Opioid analgesics administered for post-traumatic, postoperative and cancer pain.
Tricyclic antidepressants recommended for neuropathic pain.
Triptans are prescribed for the treatment of migraine headaches.
The World Health Organization (WHO) has developed a guideline for pain management. It consists of three levels of intensity. Moving to a higher tier is associated with ineffectiveness of the drug from a lower ladder or when pain increases.
Grade 1 (mild to moderate pain) is NSAIDs
II degree (moderate to severe pain) recommended weak opioid drugs
Grade III (severe to very severe pain) prescribed strong opioids.
Grade 1 non-opioid analgesics according to WHO
The characteristic profile of action and the wide scope of application put them in the first place in terms of the frequency of using pharmacological preparations. Their mechanism of action is based on the inhibition of prostaglandin synthesis – they affect their cyclooxygenase. They can be divided into two groups. The first consists of two substances, paracetamol and metamizole, which are mainly characterized by analgesic and antipyretic properties.
- PARACETAMOL is the drug of choice in the treatment of mild chronic pain ailments and is also the first-line drug in the treatment of fever, especially in the elderly, with kidney diseases, increased cardiovascular risk and increased risk of gastroenterological complications, as well as in pregnant women. Paracetamol is used in combination with NSAIDs as well as with opioids from the 2nd and 3rd degree of the analgesic ladder. Side effects include hepatotoxicity. It should also be remembered that long-term alcohol abuse with the concomitant use of acetaminophen in excessive doses may increase the risk of toxic liver damage.
Dosage up to 1000mg every 6-8 hours !. At least every 4 hours (dose 500 mg)
- METAMIZOL (Pyralgin, Pyralgina, Gardan), unlike paracetamol, has an additional non-selective spasmolytic effect, so it will be useful in the treatment of acute pain, especially visceral pain, and fever resistant to other drugs. May cause leukopenia, agranulocytosis, kidney and liver damage.
The second group will have three components of action: antipyretic, analgesic and anti-inflammatory, therefore it is called non-steroidal anti-inflammatory drugs. However, depending on the chemical structure, they are prescribed for various pharmacological purposes. This large group includes such active substances as:
ACETYL SALICYLIC ACID (Aspirin, Polopyrine, Polocard, Acard) – works well against fever
DIKLOFENAK (Diclofenac, Voltaren, Olfen) – in pain, degeneration of the joints and spine, rheumatic pains.
INDOMETATHIN (Metindol) – used in the treatment of Bartter’s syndrome, Reiter’s syndrome, rheumatoid arthritis, Paget’s disease, degeneration of the joints and spine.
KETOPROFEN (Ketonal, Ketores, Fastum) is widely used in the treatment of postoperative and traumatic pain and symptomatic treatment of inflammatory and degenerative changes in joints.
IBUPROFEN (Nurofen, Ibuprom, Metafen, Ibum, Dolgit, Modafen) – has a weak analgesic, anti-inflammatory and antipyretic effect. The safest of the NSAIDs – the weakest side effects
FLURBIPROFEN (Flurbiprofen, Strepsils Intensive, Flurbifex) – used to relieve pain of mild and moderate intensity, e.g. toothache, menstrual pain, migraine, postoperative pain and helpful in the treatment of degenerative joint diseases.
NAPROKSEN (ApoNaproxen) has a strong anti-inflammatory, analgesic and antipyretic effect. Used in rheumatoid arthritis and arthrosis. It penetrates the blood-placenta barrier.
DEKSIBUPROFEN (Seractil) for the treatment of acute menstrual pain, other types of mild to moderate pain such as musculoskeletal or dental pain, and symptomatic treatment of pain and inflammation in osteoarthritis.
MEFENAMIC ACID (Mefacit) – it is used for a short time, mainly to relieve menstrual pain. It can also be used to treat an acute attack of gout and to prevent menstrual migraines. It has the weakest anti-aggregation effect on platelets.
PIROXIKAM (Apo-Piroxicam) – in rheumatoid arthritis, degenerative and productive lesions of the spine, osteoarthritis (degenerative diseases of the joints), acute gout attack
MELOKSIKAM (Aglan, Mel, Movalis, Opokan, Trosicam, Reumelox) – in the symptomatic treatment of rheumatic and degenerative diseases (including rheumatoid arthritis).
PROPYFENAZONE (Saridon, Cefalgin) treatment of fever, pain
NABUMETON (Nabuton) – indicated in the course of osteoarthritis and rheumatoid arthritis.
NIMESULID (Nimesil) – can only be used as a second-line drug in the treatment of acute pain in dysmenorrhea.
CELEKOKSIB (Aclexa) – symptomatic treatment of inflammation and pain in osteoarthritis, rheumatoid arthritis (RA) and ankylosing spondylitis.
Side effects of NSAIDs:
– gastrointestinal disorders, from erosions to ulcers
– skin reactions – impaired kidney function – swelling and increase in blood pressure
– inhibition of platelet aggregation
– dizziness and headache
– decrease in uterine motor activity
– heart attack, stroke
– triggering an asthma attack
Interactions – Connecting:
– NSAIDs lead to an increased risk of gastrointestinal bleeding and ulcers in the digestive tract
– NSAIDs with alcohol increase the risk of gastrointestinal bleeding and hepatotoxicity (PARACETAMOL)
– NSAIDs with a blood pressure lowering drug lead to a decrease in the activity of the antihypertensive drug, thus there is a risk of heart attack, stroke, kidney failure
– NSAIDs + anti-aggregating drugs (warfarin, clopidogrel, ticlopidine) lead to a risk of bleeding
– NSAIDs + oral antidiabetic drugs (biguanide-metformin derivatives, sulfonylurea derivatives – gliclazide, glimeperide, glipizide) may inhibit the excretion of anti-diabetic drugs and, consequently, reduce blood sugar and hypoglycaemia.
– NSAIDs + antacids (PPIs, alkalizing drugs) reduce the absorption of NSAIDs and reduce the effect of NSAIDs.
Seemingly simple substances aimed at eliminating the most often bothering ailments have different applications in individual disease entities. Therefore, it is important to properly select drugs by a doctor or pharmacist in order to find a safe and effective remedy.
- Mutschler, G. Geisslinger, H. K. Kroemer, P. Ruth, Mutschler Pharmacology and Toxicology.
- Szczeklik, P. Gajewsk, Interna Szczeklik.
- Pharmacodynamics, a textbook for Students of Pharmacy
- Zygadło, (2008) interactions of the most commonly used over-the-counter painkillers, anti-inflammatory and antipyretic drugs.